TABLE 2.
Summary of testing of ADAM10 selective inhibitors with various cell-based ADAM10 and synthetic substrates.
Target | Cell line | Glycosylation type | Position | [C] tested, μM | CID3117694, %inhibition (IC50, μM) | GI254023X, %inhibition |
TNFα non-glycosylateda | N/A | None | N/A | 0.01–100 | 18 (>100) | 100 |
TNFα glycosylateda | N/A | Gal-GalNAc | S4 | 0.01–100 | 100 (1.1) | 100 |
HER2a | BT474 | GlcNAc | Multiple (Yuan et al., 2003) | 10 | 0 | 100 |
CXCL16a | A549 | Gal-GalNAc | Multiple (Abel et al., 2004) | 10 | 80 | 100 |
Syndecan-4a | A549 | Heparan Sulfate | S39, S61, S63 (Bernfield et al., 1992) | 10 | 0 | 100 |
NT, not tested. aMadoux et al. (2016).